Assay Detail
Binding
CHEMBL1787625
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]flunitrazepam from benzodiazepine binding site GABAA alpha2beta3gamma2 receptor expressed in Sf9 cells after 1 hr
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Sf9 |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; alpha-2/beta-3/gamma-2 (CHEMBL2094130) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Development and SAR of functionally selective allosteric modulators of GABAA receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 45 | 7.97 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1783282 | AZD7325 | 2.0 | 1 | 9.51 |
| CHEMBL1783284 | — | — | 1 | 9.42 |
| CHEMBL1783283 | — | — | 1 | 9.39 |
| CHEMBL1783285 | — | — | 1 | 9.25 |
| CHEMBL1783245 | — | — | 1 | 9.00 |
| CHEMBL1783276 | — | — | 1 | 9.00 |
| CHEMBL1783271 | — | — | 1 | 8.94 |
| CHEMBL1783272 | — | — | 1 | 8.79 |
| CHEMBL1783250 | — | — | 1 | 8.71 |
| CHEMBL1783280 | — | — | 1 | 8.65 |
| CHEMBL1783287 | — | — | 1 | 8.62 |
| CHEMBL1783286 | — | — | 1 | 8.54 |
| CHEMBL1783251 | — | — | 1 | 8.49 |
| CHEMBL1783273 | — | — | 1 | 8.45 |
| CHEMBL1783269 | — | — | 1 | 8.33 |
| CHEMBL1783247 | — | — | 1 | 8.26 |
| CHEMBL1783274 | — | — | 1 | 8.24 |
| CHEMBL1783281 | — | — | 1 | 8.21 |
| CHEMBL1783246 | — | — | 1 | 8.18 |
| CHEMBL1783249 | — | — | 1 | 8.14 |
| CHEMBL1783279 | — | — | 1 | 8.13 |
| CHEMBL1783248 | — | — | 1 | 8.07 |
| CHEMBL1783252 | — | — | 1 | 8.05 |
| CHEMBL1783253 | — | — | 1 | 8.00 |
| CHEMBL1783244 | — | — | 1 | 8.00 |
| CHEMBL1783266 | — | — | 1 | 7.89 |
| CHEMBL1783277 | — | — | 1 | 7.86 |
| CHEMBL1783278 | — | — | 1 | 7.86 |
| CHEMBL1783254 | — | — | 1 | 7.86 |
| CHEMBL1783265 | — | — | 1 | 7.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1783282 | AZD7325 | Ki | = | 0.309 | nM | 9.51 |
| CHEMBL1783284 | — | Ki | = | 0.3802 | nM | 9.42 |
| CHEMBL1783283 | — | Ki | = | 0.4074 | nM | 9.39 |
| CHEMBL1783285 | — | Ki | = | 0.5623 | nM | 9.25 |
| CHEMBL1783245 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1783276 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1783271 | — | Ki | = | 1.148 | nM | 8.94 |
| CHEMBL1783272 | — | Ki | = | 1.622 | nM | 8.79 |
| CHEMBL1783250 | — | Ki | = | 1.95 | nM | 8.71 |
| CHEMBL1783280 | — | Ki | = | 2.239 | nM | 8.65 |
| CHEMBL1783287 | — | Ki | = | 2.399 | nM | 8.62 |
| CHEMBL1783286 | — | Ki | = | 2.884 | nM | 8.54 |
| CHEMBL1783251 | — | Ki | = | 3.236 | nM | 8.49 |
| CHEMBL1783273 | — | Ki | = | 3.548 | nM | 8.45 |
| CHEMBL1783269 | — | Ki | = | 4.677 | nM | 8.33 |
| CHEMBL1783247 | — | Ki | = | 5.495 | nM | 8.26 |
| CHEMBL1783274 | — | Ki | = | 5.754 | nM | 8.24 |
| CHEMBL1783281 | — | Ki | = | 6.166 | nM | 8.21 |
| CHEMBL1783246 | — | Ki | = | 6.607 | nM | 8.18 |
| CHEMBL1783249 | — | Ki | = | 7.244 | nM | 8.14 |
| CHEMBL1783279 | — | Ki | = | 7.413 | nM | 8.13 |
| CHEMBL1783248 | — | Ki | = | 8.511 | nM | 8.07 |
| CHEMBL1783252 | — | Ki | = | 8.913 | nM | 8.05 |
| CHEMBL1783244 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1783253 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1783266 | — | Ki | = | 12.88 | nM | 7.89 |
| CHEMBL1783277 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL1783278 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL1783254 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL1783265 | — | Ki | = | 14.45 | nM | 7.84 |
| CHEMBL1783255 | — | Ki | = | 15.14 | nM | 7.82 |
| CHEMBL1783256 | AZD6280 | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL1783257 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL1783258 | — | Ki | = | 29.51 | nM | 7.53 |
| CHEMBL1783270 | — | Ki | = | 33.11 | nM | 7.48 |
| CHEMBL1783275 | — | Ki | = | 56.23 | nM | 7.25 |
| CHEMBL1783259 | — | Ki | = | 56.23 | nM | 7.25 |
| CHEMBL1783267 | — | Ki | = | 60.26 | nM | 7.22 |
| CHEMBL1783260 | — | Ki | = | 91.2 | nM | 7.04 |
| CHEMBL1783261 | — | Ki | = | 109.65 | nM | 6.96 |
| CHEMBL1783262 | — | Ki | = | 128.82 | nM | 6.89 |
| CHEMBL1783268 | — | Ki | = | 263.03 | nM | 6.58 |
| CHEMBL1783263 | — | Ki | = | 537.03 | nM | 6.27 |
| CHEMBL1783236 | — | Ki | = | 1862.09 | nM | 5.73 |
| CHEMBL1783264 | — | Ki | = | 3548.13 | nM | 5.45 |